GSK J4 HCl

ChemicalBook > CAS DataBase List > GSK J4 HCl

Product Name: GSK J4 HCl
CAS No.: 1373423-53-0
Chemical Name: GSK J4 HCl
Synonyms: GSK-J4;GSK J4;CS-1667;CS-2143;GSK J4 HCl;6-Triiodophenol;GSK J4 free base;GSKJ4HCL(free base);GSK J4 HCl USP/EP/BP;GSK J4 HCl (GSKJ4 HCl)
CBNumber: CB62665155
Molecular Formula: C24H27N5O2
Formula Weight: 417.5
MOL File: 1373423-53-0.mol

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GSK J4 HCl Property

Boiling point:: 581.2±50.0 °C(Predicted)
Density: 1.216±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: soluble20mg/mL, clear
form: Tan semi-solid
pka: 5.95±0.10(Predicted)
color: white to beige
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChIKey: WBKCKEHGXNWYMO-UHFFFAOYSA-N

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Safety

Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0701
Product name: GSK-J4
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $117
Updated: 2024/03/01

Sigma-Aldrich

Product number: 420205
Product name: Histone Lysine Demethylase Inhibitor VIII, GSK-J4
Packaging: 10mg
Price: $245
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0701
Product name: GSK-J4
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $469
Updated: 2024/03/01

Tocris

Product number: 4594
Product name: GSKJ4
Purity: ≥99%(HPLC)
Packaging: 50
Price: $876
Updated: 2021/12/16

TRC

Product number: G797555
Product name: GSKJ4
Packaging: 10mg
Price: $165
Updated: 2021/12/16

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GSK J4 HCl Chemical Properties,Usage,Production

Description

GSK-J4 (1373423-53-0) is a histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1 (cat.# 10-1393).1 GSK-J4 rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies.2

Uses

GSK-J4 has been used to study the effect of KDM2B (Jumonji (JmjC) domain histone 3 lysine 36 (H3K36) di-demethylase) inhibition on the survival and DNA repair potential of glioblastoma cells. It has also been used in sulforhodamine B (SRB) cell growth assay and cell viability assay.

Definition

ChEBI: 3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid ethyl ester is an organonitrogen heterocyclic compound.

Biochem/physiol Actions

GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. For characterization details for GSK-J4 and full characterization details for GSK-J1, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

storage

Room temperature

References

1) Kruidenier et al. (2012), Selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404 2) Inoue et al. (2014) New Braf knockin mice provide a pathogenic mechanism of developmental defects and therapeutic approach in cardio-facio-cutaneous syndrome; Hum. Mol. Genet.,?23?6553

GSK J4 HCl Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GSK J4 HCl manufacturers

Career Henan Chemical Co

Product: ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate 1373423-53-0
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-23

1373423-53-0, GSK J4 HClRelated Search:

2-Cyanopyridine GSK2982772 GSK2636771 Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- GSK778 N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide TRICHOSTATIN A Resveratrol RVX-208 5-Azacytidine GSK J1 GSK J5 GSK J2 BIX 01294 GSK 343 JIB-04 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol OG-L002

GSK J4

GSK-J4

N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester

GSK J4 HCl

N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyriMidinyl]-|-alanine ethyl ester

β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester, hydrochloride (1:1)

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate

ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate

CS-2143

CS-1667

H3K27 histone demethylase inhibitor J4 HCl

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem

GSK J4 free base

GSKJ4HCL(free base)

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)prop

Histone Lysine Demethylase Inhibitor VIII, GSK-J4

β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester

GSK J4 HCl USP/EP/BP

GSK J4 HCl (GSKJ4 HCl)

6-Triiodophenol

1373423-53-0

C24H27N5O2HCl

API

Inhibitor

Inhibitors